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CO4950533A1 - METHODS TO MODULATE SERINE / THREONINE PROTEIN KINASE FUNCTION WITH QUINAZOLINE BASED COMPOUNDS - Google Patents

METHODS TO MODULATE SERINE / THREONINE PROTEIN KINASE FUNCTION WITH QUINAZOLINE BASED COMPOUNDS

Info

Publication number
CO4950533A1
CO4950533A1 CO98024266A CO98024266A CO4950533A1 CO 4950533 A1 CO4950533 A1 CO 4950533A1 CO 98024266 A CO98024266 A CO 98024266A CO 98024266 A CO98024266 A CO 98024266A CO 4950533 A1 CO4950533 A1 CO 4950533A1
Authority
CO
Colombia
Prior art keywords
group
membered aryl
protein kinase
hydrogen
formula
Prior art date
Application number
CO98024266A
Other languages
Spanish (es)
Inventor
Cho Tang Peng
Gerald Mcmahon
Heinz Weinberger
Bernhard Kutscher
Harald App
Original Assignee
Sugen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sugen Inc filed Critical Sugen Inc
Publication of CO4950533A1 publication Critical patent/CO4950533A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57484—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/91—Transferases (2.)
    • G01N2333/912—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • G01N2333/91205—Phosphotransferases in general
    • G01N2333/9121—Phosphotransferases in general with an alcohol group as acceptor (2.7.1), e.g. general tyrosine, serine or threonine kinases
    • G01N2333/91215—Phosphotransferases in general with an alcohol group as acceptor (2.7.1), e.g. general tyrosine, serine or threonine kinases with a definite EC number (2.7.1.-)

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Cell Biology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un método para modular la función de una quinasa proteínicade serina y treonina con un compuesto a base de quinazolina sustituido en la posición 5 con un anillo de arilo o heteroarilo de 5 ó 6 miembros sustituido voluntariamente, el cual comprende la etapa de detección de células que secretan la ya mencionada quinasa proteínica de serina y treonina con el también mencionado compuesto. El método de reivindicación 1, en el que el compuesto mencionado base de quinazolina tiene una estructura que aparece a continuación en la fórmula I, II o III: en la que (a) Z es oxígeno, NX1 , o azufre, (donde X1 se selecciona del grupo constituido por hidrógeno, alquilo saturado o no saturado y mitades de anillos de arilo o heteroarilo de cinco o seis miembros); b) n es 0, 1, 2, 3 ó 4; (c) A1 , A2 , A3 , A4 , A5 y A6 se seleccionan separadamente del grupo constituido por carbono, nitrógeno, oxígeno y azufre; (d) R1 , R2 , R3 , R4 , R5 , R6 , R7 , R8 , R9 y R10 se seleccionan separadamente del grupo constituido por (I) hidrógeno,(II) alquilo saturado o no saturado, (III) NX2 X3 (donde X2 y X3 se seleccionan separadamente del grupo constituido por hidrógeno, alquilo saturado o no saturado y mitades de anillos de arilo o heteroarilo de cinco o seis miembros); y (IV) halógeno o trihalometilo, (V) una cetona de fórmula -CO-X4 (donde X4 se selecciona del grupo constituido por hidrógeno, alquilo y mitades de anillos de arilo o heteroarilo de cinco o seis miembros), (VI) un ácido carboxílico de fórmula -(X5 )n -COOH o éster de fórmula -(X6 )n -COO-X7 (donde X5 , X6 y X7 se seleccionan separadamente del grupo constituido por alquilo y mitades de arilo o heteroarilo de cinco o seis miembros, y en el que n es O ó 1),...A method of modulating the function of a serine and threonine protein kinase with a quinazoline-based compound substituted at the 5-position with a voluntarily substituted 5- or 6-membered aryl or heteroaryl ring, which comprises the step of detecting cells that they secrete the aforementioned serine and threonine protein kinase with the also mentioned compound. The method of claim 1, wherein said quinazoline base compound has a structure listed below in formula I, II or III: wherein (a) Z is oxygen, NX1, or sulfur, (where X1 is select from the group consisting of hydrogen, saturated or unsaturated alkyl, and 5- or six-membered aryl or heteroaryl ring moieties); b) n is 0, 1, 2, 3 or 4; (c) A1, A2, A3, A4, A5 and A6 are selected separately from the group consisting of carbon, nitrogen, oxygen and sulfur; (d) R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are selected separately from the group consisting of (I) hydrogen, (II) saturated or unsaturated alkyl, (III) NX2 X3 (where X2 and X3 are selected separately from the group consisting of hydrogen, saturated or unsaturated alkyl, and 5- or six-membered aryl or heteroaryl ring moieties); and (IV) halogen or trihalomethyl, (V) a ketone of the formula -CO-X4 (where X4 is selected from the group consisting of hydrogen, alkyl and 5- or six-membered aryl or heteroaryl ring halves), (VI) a carboxylic acid of the formula - (X5) n -COOH or ester of the formula - (X6) n -COO-X7 (where X5, X6 and X7 are selected separately from the group consisting of 5- or 6-membered aryl or heteroaryl moieties , and in which n is O or 1), ...

CO98024266A 1997-05-02 1998-05-04 METHODS TO MODULATE SERINE / THREONINE PROTEIN KINASE FUNCTION WITH QUINAZOLINE BASED COMPOUNDS CO4950533A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4535197P 1997-05-02 1997-05-02
US6015297P 1997-09-26 1997-09-26

Publications (1)

Publication Number Publication Date
CO4950533A1 true CO4950533A1 (en) 2000-09-01

Family

ID=26722670

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98024266A CO4950533A1 (en) 1997-05-02 1998-05-04 METHODS TO MODULATE SERINE / THREONINE PROTEIN KINASE FUNCTION WITH QUINAZOLINE BASED COMPOUNDS

Country Status (8)

Country Link
US (2) US6204267B1 (en)
EP (1) EP0981519A1 (en)
JP (1) JP2001524128A (en)
AR (1) AR012634A1 (en)
AU (1) AU7282998A (en)
CA (1) CA2288778A1 (en)
CO (1) CO4950533A1 (en)
WO (1) WO1998050370A1 (en)

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